Lecture 6 - Receptors and Transporters as Drug Targets Flashcards Preview

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Flashcards in Lecture 6 - Receptors and Transporters as Drug Targets Deck (21):
1

What are beta-adrenergic receptors activated by?

Catecholamines
Synthetic ligands developed to treat asthma, hypertension or cardiac disease

2

What are two catecholamines?

adrenaline and noradrenaline

3

What confers salbutamol's selectivity for the beta2 adrenergic receptor?

N-trimethyl group

4

Explain the activity of a GPCR (4)

1. Agonist binds to a receptor which induces change in receptor association alpha subunit
2. GDP is released and replaced with GTP in the alpha subunit
3. The alpha and betagamma subunits dissociate
4. The subunits modulate activity of other enzymes or ion channels

5

What does agonist binding induce in the binding pocket?

A 1 angstrom contraction of the binding pocket relative to the antagonist bound receptor

6

What do full agonists form hydrogen bonds wiht?

Two conserved serine residues in transmembrane helix 5

7

What do partial agonists interact with only?

Serine211

8

What is the difference between a passive transporter and an active transporter?

Active transporters require energy and move substrates against a concentration gradient

9

What do primary active transporters use for energy? (2)

Light, ATP hydrolysis

10

What do secondary active transporters use for energy?

Pre-existing ion gradients

11

What are two main families of neurotransmitter transporters on the pre and post synaptic neurones?

-Glutamate transporter family
-Neurotransmitter sodium symporter (NSS) family

12

What are some substrates for the NSS family? (5)

GABA, glycine, dopamine, noradrenaline, serotonin

13

What are all neurotransmitter transporters?

Secondary active transporters

14

What are the substrate of the glutamate transporter family? (2)

Glutamate and aspartate

15

What chemical gradient is the NET transporter coupled to?

Na+ and Cl-

16

What drugs target NETs (3)

TCA, SNRI and drugs of abuse (cocaine, amphetamine, meth)

17

What two transporters are found at the noradrenergic nerve terminal?

Vesicular Monoamine transporter (VMAT)
Norepinephrine Transporter (NET)

18

What has been crystallised to be used as a homologue for the NET?

Bacterial homologue, LeuTaa

19

What is the shape of the LeuTaa

Shot glass

20

What is NSS

Neurotransmitter sodium symporter

21

What site does clomipramine bind on?

Secondary binding site